Page last updated: 2024-11-11

dihydroergotoxine

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Description

Dihydroergotoxine: A mixture of three different hydrogenated derivatives of ERGOTAMINE: DIHYDROERGOCORNINE; DIHYDROERGOCRISTINE; and DIHYDROERGOCRYPTINE. Dihydroergotoxine has been proposed to be a neuroprotective agent and a nootropic agent. The mechanism of its therapeutic actions is not clear, but it can act as an alpha-adrenergic antagonist and a dopamine agonist. The methanesulfonate salts of this mixture of alkaloids are called ERGOLOID MESYLATES. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6420006
CHEMBL ID1396675
SCHEMBL ID40844
MeSH IDM0006406

Synonyms (26)

Synonym
MLS002207048
smr001230668
MLS002153175
dihydroergotamine methanesulfonate salt, powder
dihydroergotoxine
PRESTWICK_746
11032-41-0
D2633
HMS2231H03
SCHEMBL40844
CHEMBL1396675
mfcd05618219
dihydroergotamine mesylate, united states pharmacopeia (usp) reference standard
dihydroergotamine mesilate, european pharmacopoeia (ep) reference standard
910882-42-7
EN300-122619
(4r,7r)-n-[(1s,2s,4r,7s)-7-benzyl-2-hydroxy-4-methyl-5,8-dioxo-3-oxa-6,9-diazatricyclo[7.3.0.0^{2,6}]dodecan-4-yl]-6-methyl-6,11-diazatetracyclo[7.6.1.0^{2,7}.0^{12,16}]hexadeca-1(15),9,12(16),13-tetraene-4-carboxamide; methanesulfonic acid
dihydroergotamine for peak identification, european pharmacopoeia (ep) reference standard
(6ar,9r)-n-((2r,5s,10as,10bs)-5-benzyl-10b-hydroxy-2-methyl-3,6-dioxooctahydro-8h-oxazolo[3,2-a]pyrrolo[2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide methanesulfonate
(6ar,9r)-n-((2r,5s,10as,10bs)-5-benzyl-10b-hydroxy-2-methyl-3,6-dioxooctahydro-2h-oxazolo[3,2-a]pyrrolo[2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide methanesulfonate
(6ar,9r)-n-((2r,5s,10as,10bs)-5-benzyl-10b-hydroxy-2-methyl-3,6-dioxooctahydro-2h-oxazolo[3,2-a]pyrrolo[2,1-c]pyrazin-2-yl)-7-methyl-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide
(6ar,9r)-n-[(1s,2s,4r,7s)-7-benzyl-2-hydroxy-4-methyl-5,8-dioxo-3-oxa-6,9-diazatricyclo[7.3.0.02,6]dodecan-4-yl]-7-methyl-6,6a,8,9,10,10a-hexahydro-4h-indolo[4,3-fg]quinoline-9-carboxamide;methanesulfonic acid
Q16633838
HMS3886K22
F85120
dihydroergotamine for peak identification

Research Excerpts

Actions

Dihydroergotoxine did not inhibit the postsynaptic effect of isoprenaline and noradrenaline. It reduced the neurally induced pressor responses and tachycardia in the rat.

ExcerptReferenceRelevance
"Dihydroergotoxine did not inhibit the postsynaptic effect of isoprenaline and noradrenaline but reduced the neurally induced pressor responses and tachycardia in the rat."( Presynaptic inhibition by dihydroergotoxine of the response to peripheral sympathetic nerve stimulation in rats.
Grenie, B; Roquebert, J, 1987
)
1.29
"Dihydroergotoxine did not suppress the cardiovascular and plasma norepinephrine concentration."( Peripheral dopamine receptors in the antihypertensive action of dihydroergotoxine in humans.
Cherchi, A; Gessa, G; Mercuro, G; Rivano, CA; Rossetti, ZL; Ruscazio, M; Tocco, L, 1987
)
1.23

Treatment

Dihydroergotoxine treatment partially re-establishes the learning abilities in animals. At the same time, it increases the number of cholinergic receptors. This effect could explain the actions of this drug on the memory process in ageing persons.

ExcerptReferenceRelevance
"Dihydroergotoxine treatment partially suppresses the micro-infarct effects before the reestablishment of rat performance in behavioral tests."( [Learning, hemodynamic and metabolic attendant effects in aged animals after an acute ischemic accident].
Duterte, D; Galiez, V; Lamproglou, Y; Le Poncin-Lafitte, M; Rapin, JR, 1983
)
0.99
"Dihydroergotoxine treatment (25 days, 1 mg/kg body weight daily) counteracts these changes."( Key enzymes of glycolysis in rat brain: effects of single and repetitive treatment with dihydroergotoxine (Redergin).
Djuricić, BM; Mrsulja, BB, 1980
)
1.2
"Dihydroergotoxine treatment facilitated the learning performance of rats in both the original and reversal learning tests."( Effect of dihydroergotoxine, a cerebral vasodilator, on cognitive deficits induced by prenatal undernutrition and environmental impoverishment in young rats.
Bhattacharya, SK; Jaiswal, AK; Upadhyay, SN, 1991
)
1.41
"The treatment by dihydroergotoxine partially re-establishes the learning abilities in animals and, at the same time, increases the number of cholinergic receptors This effect could explain the actions of this drug on the memory process in ageing persons."( Learning and cholinergic neurotransmission in old animals: the effect of Hydergine.
Duterte, D; Galiez, V; Lamproglou, I; Le Poncin-Lafitte, M; Rapin, JR, 1985
)
0.6

Toxicity

ExcerptReferenceRelevance
" The only adverse event reported was a case of mild gastric pain at the end of treatment with 20 mg dihydroergocristine."( Comparison of the efficacy and safety of daily dosages of 6 mg and 20 mg dihydroergocristine in the treatment of chronic cerebro-vascular disease.
Galbiati, GC; Pagliano, FM,
)
0.13
" Dihydroergocryptine antagonized both the neuronal death produced by acute exposure to a toxic glutamate concentration as well as the normal age-dependent degeneration in culture."( Protection by dihydroergocryptine of glutamate-induced neurotoxicity.
Aleppo, G; Canonico, PL; Favit, A; Scapagnini, U; Sortino, MA, 1993
)
0.29

Pharmacokinetics

ExcerptReferenceRelevance
"The pharmacokinetic properties of dihydroergocristine (DHEC, CAS 17479-19-5) were investigated in rats using a specific radioimmunoassay technique specific for non-metabolized drugs."( [The pharmacokinetics of dihydroergocristine after intravenous and oral administration in rats].
Coppi, G; Grognet, JM; Istin, M; Rivière, R; Zanotti, A, 1992
)
0.28
" DHEC shows a plasma profile according to a 3-compartment pharmacokinetic model with a long half-life and high distribution volume."( [The pharmacokinetics of dihydroergocristine in free-will subjects after oral administration of three formulations].
Coppi, G; Mailland, F; Zanotti, A, 1992
)
0.28
"The pharmacokinetic profile of a single dose (6 mg/kg) of alpha-dihydroergokryptine (alpha-DHEK) was established after oral administration in monkeys using a radio-immunoassay technique for non-metabolized drug."( Pharmacokinetics of alpha-dihydroergokryptine in monkeys after oral administration.
Coppi, G; Grognet, JM; Istin, M; Mailland, F; Zanotti, A, 1991
)
0.28
"The pharmacokinetic properties of alpha-dihydroergocryptine methanesulphonate (alpha-DHEK, CAS 19467-62-0) were investigated in rat using a radioimmunoassay technique for nonmetabolized drug."( Pharmacokinetics of alpha-dihydroergocryptine in rats after intravenous and oral administration.
Coppi, G; Grognet, JM; Istin, M; Mailland, F; Zanotti, A, 1991
)
0.28
"The study was carried out to explore the potential for pharmacokinetic interaction of a single oral dose of alpha-dihydroergocryptine (CAS 14271-05-7, DHEC, Almirid) with digoxin."( Study on the interaction of the dopamine agonist alpha-dihydroergocryptine with the pharmacokinetics of digoxin.
Althaus, M; de Mey, C; Mazur, D; Retzow, A; Vens-Cappell, B, 2000
)
0.31
" In patients with impaired hepatic function, the geometric mean Cmax and AUC(0-infinity) values for unchanged DHEC were 571."( Plasma and urine pharmacokinetics of the dopamine agonist alpha-dihydroergocryptine in patients with hepatic dysfunction.
Althaus, M; de Mey, C; Ezan, E; Goszcz, A; Kostka-Trabka, E; Retzow, A, 2001
)
0.31
" The developed method was successfully applied to pharmacokinetic study of fixed dose combination of clopamide, reserpine and dihydroergotoxine in healthy male volunteers."( Validated liquid chromatography-tandem mass spectrometry method for simultaneous determination of clopamide, reserpine and dihydroergotoxine: Application to pharmacokinetics in human plasma.
Attia, KA; Demellawy, MA; Kaddah, MM; Nassar, MW; Sharaf El-Din, MM, 2016
)
0.85

Compound-Compound Interactions

ExcerptReferenceRelevance
"Using two models of experimental thrombosis (arterio-venous shunt and Wessler's model) the effect of plasmin and its combination with alpha-adrenoreceptor antagonists on the formation of thrombus was studied on white rats."( [Thrombosis prophylaxis using plasmin and its combination with alpha-adrenoreceptor antagonists].
Golubeva, MG; Grigoréva, ME; Kalishevskaia, TM,
)
0.13

Bioavailability

ExcerptReferenceRelevance
"In six healthy volunteers the bioavailability of alpha-acetyldigoxin in solution and tablet form was compared with a tablet which in addition to alpha-acetyldigoxin contained the DH-ergot alkaloid Hydergine in identical galenic formulation."( The bioavailability of alpha-acetyldigoxin from Card-Hydergin--a fixed combination of Hydergine and acetyldigoxin.
Klotz, U, 1978
)
0.26
"The relative bioavailability and plasma concentration profile of dihydroergotoxine as a solution, standard tablets and slow-release formulations have been compared in 12 healthy subjects following the application of 4-5 mg as a single dose or as 2-3 smaller dose units given at 5 h intervals."( Bioavailability of slow-release co-dergocrine mesylate (dihydroergotoxine) formulations.
Habedank, WD; Herrmann, W; Loh, W; Rietbrock, N; Woodcock, BG, 1987
)
0.76
" The therapeutic benefit that might derive from greater bioavailability of the liquid capsule has not been established."( Bioavailability of ergoloid mesylates liquid capsule.
Schran, HF, 1985
)
0.27
" The bioavailability of the retard capsule was similar to that for the solution indicating that first-pass metabolism is not significantly increased following a three-fold prolongation in the absorption rate constant."( Absorption kinetics of dihydroergotoxine following oral administration to man.
Habedank, WD; Loh, W; Rietbrock, N; Woodcock, BG, 1985
)
0.58
" The knowledge of pharmacokinetics give essential informations for the development of new pharmaceutical forms, adjustment of dosage regimen and recommendations for drug intake in order to minimize the variations in bioavailability and to improve compliance."( [Pharmacokinetics: a contribution in clinical geriatric pharmacology?].
Humbert, H; Kiechel, JR; Lavène, D, 1983
)
0.27
"An indirect method to assess bioavailability of dihydroergocristine-methansulfonate (DEC) is described."( Measuring the inhibition of TRH-stimulated prolactin by dihydroergocristine (DEC) in man: an indirect assessment of bioavailability.
Albrecht, H; Lücker, PW; Mailland, F; Venitz, J, 1984
)
0.27
"The relative bioavailability of the newly developed formulation of co-dergocrine mesylate (Hydergine special, 1 x 4 mg) was determined in elderly patients under steady state conditions, with conventional Hydergine forte tablets (2 x 2 mg) as a reference."( Steady state bioavailability of a new oral formulation of Hydergine in geriatric patients.
Abisch, E; Dennler, HJ; Lang, E; Sörgel, F, 1984
)
0.27
" The low bioavailability (19%) and the biliary recycling of DHT-equivalent material suggest a first pass effect."( Plasma kinetics of dihydroergotoxin in rat by using a radioreceptor assay.
Palmi, M; Segre, G, 1984
)
0.27
" The bioavailability of the formulation Redergin oral tablet is only a few percent lower than that of Redergin solution."( Comparison of the bioavailability of Redergin tablets (1.0 mg) and Redergin solution.
Kopitar, Z; Milovac, J; Tadjer, I; Vrhovac, B, 1982
)
0.26
" In both cases, the areas under the curves were very similar but the relative bioavailability of DHET in these two forms is very different if one considers the two components of availability extent and rate."( Comparative blood level of dihydroergotoxine (DHET) after administration of two oral forms (solution & tablet): a preliminary study.
Aliache, JM; Briot, M; Couquelet, J; Vigo, P, 1981
)
0.56
" The bioavailability of DHETM was investigated in a cross-over study on 20 male healthy volunteers to whom two single doses of 9 mg DHETM were administered either in tablets (Orphol spezial) or in oral solution (Orphol forte)."( Bioavailability and pharmacokinetic profile of dihydroergotoxine from a tablet and from an oral solution formulation.
Kozak, I; Mazur, D; Rovati, LC; Schmid, K; Setnikar, I; Vens-Cappell, B, 2001
)
0.57

Dosage Studied

In 14 patients with senile dementia, a study was made of two dosage levels (3 mg or 6 mg daily) of dihydroergotoxine mesylate. The analysis of the drug substance or its dosage forms can be carried out in about 15 min.

ExcerptRelevanceReference
" The authors show that the association of neuroleptic drugs has here also an effect of economy of dosage and facilitates the rise in blood pressure."( [Controlled arterial hypotension produced by nitroprusside combined with neuroleptics].
Bauvin, MJ; Campan, L; Clergue, ML, 1976
)
0.26
" The analysis of dihydroergotoxine mesylate drug substance or its dosage forms can be carried out in about 15 min."( Dihydroergotoxine: separation and determination of four components by high-performance liquid chromatography.
Ableidinger, W; Bethke, H; Hartmann, V; Rödiger, M, 1978
)
2.04
" The authors concluded that, at least with the dosage used in this study, none of the treatments proved more useful than conventional supportive therapy in the first 10 days after a stroke."( Is there a real treatment for stroke? Clinical and statistical comparison of different treatments in 300 patients.
Martinotti, R; Porro, F; Randazzo, A; Santambrogio, S; Sardella, F,
)
0.13
"In 14 patients with senile dementia, a study was made of two dosage levels (3 mg or 6 mg daily) of dihydroergotoxine mesylate (DEM, Hydergine)."( Dihydroergotoxine: 6-mg versus 3-mg dosage in the treatment of senile dementia. Preliminary report.
Burian, E; Hollister, LE; Yesavage, JA, 1979
)
1.92
" The daily dosage was 3 mg of Hydergin."( [Treatment of organic brain psychosyndrom in the old age. A double blind study with Hydergin (author's transl)].
Biel, ML; Seus, R; Struppler, A, 1976
)
0.26
" Blood pressure reduction was still significant in both groups during the early morning hours at the end of the dosage interval."( Influence of co-dergocrine mesilate/nifedipine compared to mefruside/nifedipine on circadian blood pressure in patients with essential hypertension.
Heintz, B; Heller, A; Kirsten, R; Nelson, K, 1990
)
0.28
" In reference to placebo, the increase of N2-P300 amplitude after the highest dosage of TEN, as well as after CDM, amounted to approximately 5 microV, which confirms the hypothesis that nootropic drugs may influence the P300 amplitude in the sense of an improved availability of cognitive processing resources."( Psychophysiological research in psychiatry and neuropsychopharmacology. II. The investigation of antihypoxidotic/nootropic drugs (tenilsetam and co-dergocrine-mesylate) in elderlies with the Viennese Psychophysiological Test-System (VPTS).
Anderer, P; Presslich, O; Resch, F; Saletu, B; Schuster, P; Semlitsch, HV, 1989
)
0.28
" Forty randomly grouped children of either sex were given an increasing dosage of codergocrine mesylate and followed up for 12 weeks."( Clinical efficacy of codergocrine mesylate in children with learning difficulties.
Bashir, A; Hussain, T; Saeed, K; Tareen, KI,
)
0.13
" The dose-effect curve for the adult rats was similar in shape to that for the aged rats, but the peak was much lower and occurred at the lowest dosage (0."( Effects of prolonged co-dergocrine mesylate (Hydergine) treatment on local cerebral glucose uptake in aged Fischer 344 rats.
Meier-Ruge, W, 1986
)
0.27
"Moderate improvement of cognitive function has been reported in many clinical studies of Hydergine (HYD) but in only a few controlled dose-response studies in animals."( Hydergine enhances memory in mice.
Cherkin, A; Flood, JF; Smith, GE, 1985
)
0.27
"5 micrograms/kg/min dosage is by itself able to give this maximum effect without any major consequences on HR, AP and MVF."( Comparison of the influence of dihydroergotoxine on cerebral oxygenation in the normoxic and hypercapnic hypoxic dog.
Allain, H; Bentué-Ferrer, D; Feuillu, A; Milon, D; Pape, D; Reymann, JM; Van den Driessche, J, 1985
)
0.56
" It is suggested that further work could be undertaken with a longer period of treatment, and at a higher dosage level of co-dergocrine, in a younger patient sample."( Co-dergocrine (hydergine) in the treatment of tardive dyskinesia.
Blowers, AJ; Gibson, AC; Rastogi, SC, 1982
)
0.26
" administration of lisuride at the dosage known to be ineffective on the postsynaptic dopamine receptor."( [Suppressive effects of lisuride on the synthesis, release and metabolism of dopamine in rat brain].
Azuma, H; Iwai, K; Kikuta, M; Liu, HJ; Oshino, N; Sato, K, 1982
)
0.26
" Postsynaptic alpha-adrenoceptor antagonist activity was assessed by comparing cumulative noradrenaline and phenylephrine dose-response curves in the absence and in the presence of increasing concentrations of antagonist."( [Action of dihydroergocristine at pre- and postsynaptic alpha-adrenoceptors in the rat isolated vas deferens].
Demichel, P; Gomond, P; Malek, A; Roquebert, J,
)
0.13
" The knowledge of pharmacokinetics give essential informations for the development of new pharmaceutical forms, adjustment of dosage regimen and recommendations for drug intake in order to minimize the variations in bioavailability and to improve compliance."( [Pharmacokinetics: a contribution in clinical geriatric pharmacology?].
Humbert, H; Kiechel, JR; Lavène, D, 1983
)
0.27
" DHEC antagonized 5-HT in a non competitive manner, shifting to the right and flattening the dose-response curves of this agonist."( Inhibition of norepinephrine- and 5-hydroxytryptamine-induced contraction on rat aorta by dihydroergocristine.
D'Agostino, G; Dondi, G; Grana, E; Zonta, F, 1984
)
0.27
" Therefore, Ergocomb, in the form of swallowable tablets, is considered suitable for application to patients with senile cerebral insufficiency, the recommended dosage being 3 x 1 mg."( [The use of Ergocomb in symptoms of cerebrovascular insufficiency].
Hansen, H; Pöthig, D; Sauer, I; Weidnitzer, M,
)
0.13
"2 SD after dosing with 3H-DHEC (0."( The effect of caffeine on the absorption of 3H-dihydroergocryptine (DHEC) in the rat.
Ballard, SA; Chasseaud, LF; Down, WH, 1980
)
0.26
" DEM was administered orally to 21 moderately demented subjects, in a dosage of 1 mg three times daily; and SC or CT was conducted for one hour every two weeks for a total of 12 weeks."( Senile dementia: combined pharmacologic and psychologic treatment.
Rush, L; Westphal, J; Yesavage, JA, 1981
)
0.26
" On the contrary, after ingestion of a slow-release tablet of DHET, the plasma levels took 6 hours to reach the maximum due to the slow release of the drug from this dosage form."( Comparative blood level of dihydroergotoxine (DHET) after administration of two oral forms (solution & tablet): a preliminary study.
Aliache, JM; Briot, M; Couquelet, J; Vigo, P, 1981
)
0.56
" Intraocular pressure responses to drug vehicle and 5 different doses of topical dihydroergocristine were studied in order to obtain a dose-response curve."( The effect of topical dihydroergocristine on the intraocular pressure in alpha-chymotrypsin-induced ocular hypertensive rabbits.
Melena, J; Santafé, J; Segarra, J, 1998
)
0.3
" The observed range of effects on the pharmacokinetics of DHEC in patients with compromized hepatic function does not suggest the need to revise the dosage recommendations, since treatment with DHEC is generally started with low doses and is slowly up-titrated according to the individual response and the occurrence of adverse effects."( Plasma and urine pharmacokinetics of the dopamine agonist alpha-dihydroergocryptine in patients with hepatic dysfunction.
Althaus, M; de Mey, C; Ezan, E; Goszcz, A; Kostka-Trabka, E; Retzow, A, 2001
)
0.31
"5) times the maximum observed plasma drug concentration and the area under the time course of the plasma concentrations up to the last quantifiable concentration after dosing of unchanged DHEC (determined by radioimmunoassay)."( Erythromycin increases plasma concentrations of alpha-dihydroergocryptine in humans.
Althaus, M; de Mey, C; Ezan, E; Retzow, A, 2001
)
0.31
" The trial included 5475 patients treated with vasobral in dosage 2 ml (1 ml contains 1 mg of alpha-dihydroergocryptine and 10 mg of caffeine) twice a day during 2 months."( [Preventive treatment of migraine with vasobral: a multicenter trial].
Azimova, IuE; Tabeeva, GR, 2010
)
0.36
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency12.58930.044717.8581100.0000AID485341
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency56.23410.631035.7641100.0000AID504339
acid sphingomyelinaseHomo sapiens (human)Potency19.952614.125424.061339.8107AID504937
TDP1 proteinHomo sapiens (human)Potency23.72460.000811.382244.6684AID686978; AID686979
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency28.18380.035520.977089.1251AID504332
serine-protein kinase ATM isoform aHomo sapiens (human)Potency35.48130.707925.111941.2351AID485349
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency44.66840.354828.065989.1251AID504847
importin subunit beta-1 isoform 1Homo sapiens (human)Potency100.00005.804836.130665.1308AID540263
snurportin-1Homo sapiens (human)Potency100.00005.804836.130665.1308AID540263
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1Homo sapiens (human)Potency35.48130.425612.059128.1838AID504891
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency0.09200.004611.374133.4983AID624296
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
fatty acid synthaseHomo sapiens (human)IC50 (µMol)12.43500.16605.647218.2000AID624326; AID624327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC50 (µMol)92.45300.13203.30049.5690AID624499
5-hydroxytryptamine receptor 2AMus musculus (house mouse)EC50 (µMol)36.85200.00381.36218.3930AID624503
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,042)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990913 (87.62)18.7374
1990's100 (9.60)18.2507
2000's16 (1.54)29.6817
2010's11 (1.06)24.3611
2020's2 (0.19)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 38.38

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index38.38 (24.57)
Research Supply Index7.17 (2.92)
Research Growth Index4.00 (4.65)
Search Engine Demand Index60.47 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (38.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials152 (13.23%)5.53%
Reviews43 (3.74%)6.00%
Case Studies16 (1.39%)4.05%
Observational1 (0.09%)0.25%
Other937 (81.55%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
An Exploratory Single Blind Study of Ergoloid Mesylates, 5-Hydroxytryptophan, and the Combination in Adult Males With Fragile X Syndrome [NCT05030129]Phase 215 participants (Actual)Interventional2021-10-07Completed
A Randomized, Double-Blind, Double-Dummy, Active-Controlled, Parallel, Comparative, Multicenter, Phase II Study to Evaluate the Efficacy and Safety of STA-1 Capsule in Patients With Vascular Dementia (Marrow-Sea Deficiency) [NCT01475578]Phase 2240 participants (Actual)Interventional2002-03-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]